TABLE 5

Allosteric effects of berberine on MDZ hydroxylation by recombinant CYP3A5

Values denote means ± S.D. of three separate experiments. Km and Ki are given in micromolar; Vmax is in picomoles per minute per picomole CYP3A5; Vmax/Km is in microliters per minute per picomole CYP3A5.

Berberine1′-Hydroxy MDZ4-Hydroxy MDZ
(μM)KmVmaxVmax/KmKmVmaxVmax/Km
01.55 ± 0.1859.3 ± 12.538.5 ± 12.912.6 ± 2.714.9 ± 2.61.20 ± 0.09
51.55 ± 0.5058.7 ± 8.941.6 ± 19.320.5 ± 4.114.1 ± 2.30.69 ± 0.07
251.11 ± 0.1058.2 ± 14.351.5 ± 9.739.4 ± 4.912.4 ± 2.10.32 ± 0.09
501.01 ± 0.1556.3 ± 12.154.7 ± 10.860.5 ± 5.811.4 ± 2.80.19 ± 0.05
1000.91 ± 0.1153.9 ± 11.558.9 ± 15.4100 ± 2810.0 ± 3.30.10 ± 0.02